Cancer Stem Cells

Nesuparib (JPI-547) is the orally active inhibitor for PARP 1/2 and Tankyrase 1/2 that inhibits tankyrases 1, tankyrases 2, and PARP 1 with IC₅₀s of 5, 1 and 2 nM, respectively. Nesuparib exhibits antitumor activity and can be used in research of advanced solid tumor.

Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.

Astringin (trans-Astringin) is an orally active natural phenolic stilbene glucoside. Astringin can inhibit the production of oxidative stress, inflammatory factors, etc. Astringin has multiple activities such as anti-oxidation, anti-inflammation, and anti-apoptosis. Astringin is also an inhibitor of ferroptosis. Astringin can be used in the research of diseases such as acute lung injury.

5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. 5-FAM-GpYLPQTV-NH2 can be used in cancer research.

Lasiokaurin is an anticancer agent. Lasiokaurin can be isolated from Rabdosia rubescens (Hemsl.) H. Hara. Lasiokaurin inhibits the function of the PDPK1-AKT axis, with a K_d value of 75.93 μM for PDPK1. Lasiokaurin inhibits mTOR, STAT3, MAPK and NF-κB. Lasiokaurin reduces the mRNA and protein expression levels of PLK1. Lasiokaurin decreases DNA synthesis levels, induces cell Apoptosis, and regulates Autophagy processes. Lasiokaurin inhibits tumor growth in xenograft models. Lasiokaurin can be used in research related to nasopharyngeal carcinoma, triple-negative breast cancer.

CSNK1-IN-2 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC₅₀ values of 44 nM. CSNK1-IN-2 can be used for the research of proliferative disorders.

Stemregenin 1 (SR1) (GMP) is a GMP-grade Stemregenin 1 (HY-15001). GMP-grade small molecules can be used as adjuvants in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with an IC₅₀ of 127 nM. Stemregenin 1 (GMP) can competitively bind to AhR and inhibit its nuclear translocation, inhibiting osteoclastogenesis and promoting hematopoietic progenitor cell expansion by blocking the AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway. Stemregenin 1 (GMP) can be used for the study of osteoporosis, in vitro expansion of hematopoietic stem cells, and the study of the mechanism of bone metabolic diseases.

Withanolide B is an active component of W. somnifera Dunal. Withanolide B promotes osteogenic differentiation of hBMSCs via ERK1/2 and Wnt/β-catenin signaling pathways. Withanolide B exhibits neuroprotective, anti-arthritic, anti-aging and anti-cancer effects.

CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (K_i of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC₅₀s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with K_is of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.

ar-Turmerone ((+)-ar-Turmerone) is an orally active and major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities. ar-Turmerone induces apoptosis in U937 cells. ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation in vitro and in vivo, and can be used for various neurologic disorders study.

PROTAC STAT6 degrader-1 (Compound I-2) is a potent STAT6 PROTAC degrader with a DC₅₀ <1 nM. PROTAC STAT6 degrader-1 inhibits STAT6 activity with an IC₅₀ of <0.1 pM. PROTAC STAT6 degrader-1 can be used for inflammatory and cancers research, such as non-small cell lung cancer (NSCLC).

GRGDSPC TFA, a 7-amino acid peptide, is a thiolated cell adhesion peptide.

Alcudacigib (ASP1570; DGKζ-IN-1) TFA is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC₅₀ of 4.7 nM against human DGKζ and an IC₅₀ of 3.0 nM against mouse DGKζ. Alcudacigib TFA selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib TFA enhances the anti-tumor functions of T cells and NK cells. Alcudacigib TFA can be used for the research of advanced/metastatic solid tumors.

Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc.

2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin.

STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma.

(E/Z)-Zotiraciclib ((E/Z)-TG02) is an orally active inhibitor of CDK2, JAK2 and FLT3 with IC₅₀s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer.

UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC₅₀ of 1.1 nM (Morrison K_i = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC₅₀ = 60 nM, AXL IC₅₀ = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.

3-epi-Vitamin D3 (Epicholecalciferol) (Compound 4), a Vitamin D3 analogue, is a Hedgehog pathway inhibitor with an IC₅₀ of 39.2 μM measured in U87MG cells.

A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a K_i of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain. A 1070722 decreases spontaneous locomotion.